PF 429242 dihydrochloride

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Cat.No. 3354 - PF 429242 dihydrochloride | C25H35N3O2.2HCl | CAS No. 2248666-66-0
Description: Competitive inhibitor of SREBP site 1 protease
Chemical Name: 4-[(Diethylamino)methyl]-N-[2-(2-methoxyphenyl)ethyl]-N-(3R)-3-pyrrolidinylbenzamide dihydrochloride
Purity: ≥97% (HPLC)
Datasheet
Citations (4)
Reviews
Literature
Pathways

Biological Activity

Reversible, competitive inhibitor of sterol regulatory element-binding protein (SREBP) site 1 protease (IC50 = 0.175 μM). Selective for site 1 protease against a panel of serine proteases. Inhibits rate of cholesterol synthesis in CHO cells (IC50 = 0.53 μM). Also displays antiviral activity. Cell permeable.

Licensing Information

Sold for research purposes under agreement from Pfizer Inc.

Compound Libraries

PF 429242 dihydrochloride is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 482.49
Formula C25H35N3O2.2HCl
Storage Desiccate at RT
Purity ≥97% (HPLC)
CAS Number 2248666-66-0
PubChem ID 90488837
InChI Key GSUZWFZKTIOWTI-MQWQBNKOSA-N
Smiles O=C(C2=CC=C(CN(CC)CC)C=C2)N(CCC3=CC=CC=C3OC)[C@@H]1CCNC1.Cl.Cl

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
water 24.12 50
DMSO 24.12 50

Preparing Stock Solutions

The following data is based on the product molecular weight 482.49. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.5 mM 4.15 mL 20.73 mL 41.45 mL
2.5 mM 0.83 mL 4.15 mL 8.29 mL
5 mM 0.41 mL 2.07 mL 4.15 mL
25 mM 0.08 mL 0.41 mL 0.83 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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References

References are publications that support the biological activity of the product.

Hay et al (2007) Aminopyrrolidineamide inhibitors of site-1 protease. Bioorg.Med.Chem.Lett. 17 4411 PMID: 17583500

Hawkins et al (2008) Pharmacologic inhibition of site 1 protease activity inhibits sterol regulatory element-binding protein processing and reduces lipogenic enzyme gene expression and lipid synthesis in cultured cells and experimental animals. J.Pharmacol.Exp.Ther. 326 801 PMID: 18577702

Urata et al (2011) Antiviral activity of a small-molecule inhibitor of arenavirus glycoprotein processing by the cellular site 1 protease. J.Virol. 85 795 PMID: 21068251

Olmstead (2012) Human subtilase SKI-1/S1P is a master regulator of the HCV lifecycle and a potential host cell target for developing indirect-acting antiviral agents. PLoS.Pathog. 8 e1002468 PMID: 22241994


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View all SREBP Inhibitors

Keywords: PF 429242 dihydrochloride, PF 429242 dihydrochloride supplier, SREBP, sterol, regulatory, element, binding, proteins, inhibitors, inhibits, site, 1, proteases, S1P, serine, antivirals, PF429242, Other, Proteases, Antivirals, 3354, Tocris Bioscience

4 Citations for PF 429242 dihydrochloride

Citations are publications that use Tocris products. Selected citations for PF 429242 dihydrochloride include:

Uchida et al (2016) Suppressive effects of the site 1 protease (S1P) inhibitor, PF-429242, on dengue virus propagation. Viruses 8 E46 PMID: 26875984

Kleinfelter et al (2015) Haploid Genetic Screen Reveals a Profound and Direct Dependence on Cholesterol for Hantavirus Membrane Fusion. Ann Rheum Dis 6 e00801 PMID: 26126854

Scott et al (2018) TFAP2 transcription factors are regulators of lipid droplet biogenesis. Elife 7 PMID: 30256193

Urata et al (2015) Analysis of Assembly and Budding of Lujo Virus. J Virol 90 3257 PMID: 26719243


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Literature in this Area

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Cancer

Cancer Research Product Guide

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Cancer Metabolism

Cancer Metabolism Poster

Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the main targets for cancer metabolism researchers. Genetic changes and epigenetic modifications in cancer cells alter the regulation of cellular metabolic pathways. These distinct metabolic circuits could provide viable cancer therapeutic targets.

Cardiovascular

Cardiovascular Poster

Cardiovascular disease remains one of the major causes of morbidity and mortality in the Western world and therefore this therapeutic area continues to be of great interest to researchers. This poster highlights the key GPCRs regulating vascular reactivity.

Pathways for PF 429242 dihydrochloride

Insulin

Insulin Signaling Pathway

Signaling through the insulin pathway is fundamental for the regulation of intracellular glucose levels. This pathway can become dysregulated in diabetes.